title: Development, characterization, and in vitro and in vivo evaluation of benzocaine- and lidocaine-loaded nanostructrured lipid carriers.
abstract: The present study concerns the in vitro and in vivo evaluation of benzocaine (BENZO) and lidocaine (LIDO) topical delivery from nanostructured lipid carriers (NLCs). Morphology and dimensional distribution of NLCs have been, respectively, characterized by differential scanning calorimetry (DSC) and photon correlation spectroscopy. The release pattern of BENZO and LIDO from NLCs was evaluated in vitro determining drug percutaneous absorption through excised human skin. Radiant heat tail-flick test was carried out in mice to determine the antinociceptive effect of BENZO and LIDO from NLC. DSC studies revealed that the inner oil phase of NLC plays a significant role in stabilizing the particle architecture and increasing the drug solubility. In vitro evidences show that BENZO and LIDO, when incorporated in viscosized NLC dispersions, exhibited a lower flux with respect to formulations containing the free drugs in the aqueous phase. In vivo study enabled to demonstrate that BENZO and LIDO can be released in a prolonged fashion when incorporated into lipid carriers. The results obtained pointed out NLC capability to act as an effective drug reservoir, thus prolonging the anesthetic effect of BENZO and LIDO.
authors.affiliation: Department of Pharmaceutical Sciences, University of Catania, Catania, Italy. capuglia@unict.it
authors.forename: Carmelo
authors.initials: C
authors.lastname: Puglia
authors.forename: Maria Grazia
authors.initials: MG
authors.lastname: Sarpietro
authors.forename: Francesco
authors.initials: F
authors.lastname: Bonina
authors.forename: Francesco
authors.initials: F
authors.lastname: Castelli
authors.forename: Magda
authors.initials: M
authors.lastname: Zammataro
authors.forename: Santina
authors.initials: S
authors.lastname: Chiechio
mesh_terms: D000700:Analgesics / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D001566:Benzocaine / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008012:Lidocaine / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008055:Lipids / Q000737:chemistry*; D008297:Male; D051379:Mice; D049329:Nanostructures / Q000737:chemistry; D010146:Pain / Q000188:drug therapy; D012867:Skin / Q000378:metabolism*
chemical_list: D000700:Analgesics; D000779:Anesthetics, Local; D004337:Drug Carriers; D008055:Lipids; D008012:Lidocaine; D001566:Benzocaine